23165-62-0Relevant articles and documents
Synthesis of new 3-(2-mercapto-4-oxo-4H-quinazolin-3-yl)-benzenesulfonamides with strong inhibition properties against the tumor associated carbonic anhydrases IX and XII
Bozdag, Murat,Alafeefy, Ahmed Mahmoud,Altamimi, Abdul Malik,Carta, Fabrizio,Supuran, Claudiu T.,Vullo, Daniela
, p. 2782 - 2788 (2017)
We report a series of novel metanilamide-based derivatives 3a–q bearing the 2-mercapto-4-oxo-4H-quinazolin-3-yl moiety as tail. All compounds were synthesized by means of straightforward condensation procedures and were investigated in vitro for their inh
Diversity-orientated synthesis of 3,5-bis(arylamino)pyrazoles
Degorce, Sébastien,Jung, Frédéric H.,Harris, Craig S.,Koza, Patrice,Lecoq, Jonathan,Stevenin, Arnaud
supporting information; experimental part, p. 6719 - 6722 (2012/01/05)
The synthesis of differentially-substituted 3,5-bis(arylamino)pyrazoles has not yet been documented. During our investigation, we managed to develop a novel, entirely combinatorial synthesis of 3,5-bis(arylamino)pyrazoles relying on a simple one-pot two-step operation.
Isothiazoles as active-site inhibitors of HCV NS5B polymerase
Yan, Shunqi,Appleby, Todd,Gunic, Esmir,Shim, Jae Hoon,Tasu, Tania,Kim, Hongwoo,Rong, Frank,Chen, Huaming,Hamatake, Robert,Wu, Jim Z.,Hong, Zhi,Yao, Nanhua
, p. 28 - 33 (2007/10/03)
Isothiazole analogs were discovered as a novel class of active-site inhibitors of HCV NS5B polymerase. The best compound has an IC50 of 200 nM and EC50 of 100 nM, which is a significant improvement over the starting inhibitor (1). The X-ray complex structure of 1 with HCV NS5B was obtained at a resolution of 2.2 A, revealing that the inhibitor is covalently linked with Cys 366 of the 'primer-grip'. Furthermore, it makes considerable contacts with the C-terminus, β-loop, and more importantly, to the active-site of the enzyme. The uniqueness of this binding mode offers a new insight for the rational design of novel inhibitors for HCV NS5B polymerase.
